AU2009233829A1 - Crystalline salt forms of antifolate compounds and methods of manufacturing thereof - Google Patents

Crystalline salt forms of antifolate compounds and methods of manufacturing thereof Download PDF

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Publication number
AU2009233829A1
AU2009233829A1 AU2009233829A AU2009233829A AU2009233829A1 AU 2009233829 A1 AU2009233829 A1 AU 2009233829A1 AU 2009233829 A AU2009233829 A AU 2009233829A AU 2009233829 A AU2009233829 A AU 2009233829A AU 2009233829 A1 AU2009233829 A1 AU 2009233829A1
Authority
AU
Australia
Prior art keywords
compound
optionally substituted
enantiomer
antifolate
salt
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
AU2009233829A
Other languages
English (en)
Inventor
Karol Horvath
Mikhail Lebedev
Harish K. Pimplaskar
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Chelsea Therapeutics Inc
Original Assignee
Chelsea Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Chelsea Therapeutics Inc filed Critical Chelsea Therapeutics Inc
Publication of AU2009233829A1 publication Critical patent/AU2009233829A1/en
Abandoned legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
AU2009233829A 2008-04-07 2009-04-07 Crystalline salt forms of antifolate compounds and methods of manufacturing thereof Abandoned AU2009233829A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US4299808P 2008-04-07 2008-04-07
US4299408P 2008-04-07 2008-04-07
US61/042,998 2008-04-07
US61/042,994 2008-04-07
PCT/US2009/039792 WO2009126639A1 (en) 2008-04-07 2009-04-07 Crystalline salt forms of antifolate compounds and methods of manufacturing thereof

Publications (1)

Publication Number Publication Date
AU2009233829A1 true AU2009233829A1 (en) 2009-10-15

Family

ID=40749240

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2009233829A Abandoned AU2009233829A1 (en) 2008-04-07 2009-04-07 Crystalline salt forms of antifolate compounds and methods of manufacturing thereof

Country Status (10)

Country Link
US (2) US20090253720A1 (ja)
EP (2) EP2282740A1 (ja)
JP (2) JP2011516560A (ja)
KR (1) KR20100132061A (ja)
CN (1) CN101981014A (ja)
AU (1) AU2009233829A1 (ja)
BR (1) BRPI0909198A2 (ja)
CA (2) CA2718330A1 (ja)
MX (2) MX2010010999A (ja)
WO (2) WO2009126639A1 (ja)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009126639A1 (en) * 2008-04-07 2009-10-15 Chelsea Therapeutics, Inc. Crystalline salt forms of antifolate compounds and methods of manufacturing thereof
CA2767257A1 (en) * 2009-07-08 2011-01-13 Chelsea Therapeutics, Inc. Stable crystalline polymorphs of the dipotassium salt of (s)-2-{4-[2-(2,4-diamino-quinazolin-6-yl)-ethyl]-benzoylamino}-4-methylene-penta nedioic acid
WO2011056957A2 (en) * 2009-11-06 2011-05-12 Chelsea Therapeutics, Inc. Enzyme inhibiting compounds
US20110237609A1 (en) * 2010-03-29 2011-09-29 Chelsea Therapeutics, Inc. Antifolate compositions
WO2012056285A1 (en) * 2010-10-25 2012-05-03 Fresenius Kabi Oncology Ltd. An improved process for the preparation of pemetrexed
WO2012078708A1 (en) 2010-12-07 2012-06-14 Chelsea Therapeutics, Inc. Combination comprising methotrexate and an antifolate compound
FR2969158B1 (fr) 2010-12-15 2013-01-18 Arkema France Procede pour modifiants chocs et composition thermoplastique modifiee choc ayant une resistance hydrolytique amelioree
FR2969167B1 (fr) 2010-12-15 2013-01-11 Arkema France Composition thermoplastique modifiee choc amelioree
FR2969161B1 (fr) 2010-12-15 2014-06-06 Arkema France Nouvelle poudre de polymere multi-etape coeur-ecorce, son procede de fabrication et composition comprenant celle-ci
US20130018062A1 (en) * 2011-07-12 2013-01-17 Nair Madhavan G Pain therapy with metabolism blocked antifolates
TW201700458A (zh) * 2015-04-24 2017-01-01 第一三共股份有限公司 二羧酸化合物之製法
TW202329972A (zh) 2016-08-10 2023-08-01 瑞士商赫孚孟拉羅股份公司 包含Ａｋｔ蛋白質激酶抑制劑之醫藥組合物
CN116209476A (zh) 2020-07-06 2023-06-02 拜奥迪斯私人有限公司 抗叶酸剂接头-药物和抗体-药物缀合物
WO2023126297A1 (en) 2021-12-30 2023-07-06 Byondis B.V. Antifolate linker-drugs and antibody-drug conjugates

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4818753A (en) * 1987-09-18 1989-04-04 Sri International Synthesis and method of use for 2, 4 diaminoquinazoline
NO169490C (no) * 1988-03-24 1992-07-01 Takeda Chemical Industries Ltd Analogifremgangsmaate for fremstilling av terapeutisk aktive pyrrolopyrimidinderivater
US4996206A (en) * 1989-12-11 1991-02-26 The Trustees Of Princeton University N-(pyrrolo[2,3-d]pyrimidin-3-ylacyl)-glutamic acid derivatives
KR0162654B1 (ko) * 1989-12-11 1998-11-16 알렌 제이. 시니스갤리 N-(피롤로[2,3-d]피리미딘-3-일아크릴)-글루타민산 유도체
US5248775A (en) * 1989-12-11 1993-09-28 The Trustees Of Princeton University Pyrrolo(2,3-d)pyrimidines
US5073554A (en) * 1990-01-18 1991-12-17 Nair Madhavan G Two non-polyglutamatable antifolates
US4996207A (en) * 1990-01-18 1991-02-26 Nair Madhavan G Three new non-polyglutamatable deazaaminopterins
US5508281A (en) * 1991-04-08 1996-04-16 Duquesne University Of The Holy Ghost Derivatives of pyrido [2,3-d] and [3,2-d] pyrimidine and methods of using these derivatives
IL108630A0 (en) * 1993-02-18 1994-05-30 Fmc Corp Insecticidal substituted 2,4-diaminoquinazolines
US5550128A (en) * 1994-09-09 1996-08-27 Nair; Madhavan G. Enantiomers of gamma methylene 10-deaza aminopterin and process for preparing the same
US5593999A (en) * 1995-06-07 1997-01-14 Nair; Madhavan G. Non-classical folate analogue inhibitors of glycinamide ribonucleotide formyltransferase (GARFT)
EP1001799B1 (de) * 1997-07-07 2001-10-31 PTC Pharma AG Pharmazeutische zusammensetzung enthaltend peptichemio
US5912251A (en) * 1998-01-17 1999-06-15 Nair; Madhavan G. Metabolically inert anti-inflammatory and anti-tumor antifolates
US6048736A (en) * 1998-04-29 2000-04-11 Kosak; Kenneth M. Cyclodextrin polymers for carrying and releasing drugs
AU2001259306A1 (en) * 2000-05-02 2001-11-12 Advanced Medicine, Inc. Pharmaceutical compositions containing a glycopeptide antibiotic and a cyclodextrin
NZ525573A (en) * 2000-11-28 2005-08-26 Genentech Inc LFA-1 antagonist compounds
KR100685917B1 (ko) * 2000-12-27 2007-02-22 엘지.필립스 엘시디 주식회사 전계발광소자 및 그 제조방법
US20030181635A1 (en) * 2002-03-22 2003-09-25 Harry Kochat Process for coupling amino acids to an antifolate scaffold
US20040092739A1 (en) * 2002-11-13 2004-05-13 Zejun Xiao Process for synthesizing antifolates
US7060825B2 (en) * 2003-07-25 2006-06-13 Bionumerik Pharmaceuticals, Inc. Process for synthesizing 6-quinazolinyl-ethyl-benzoyl and related antifolates
US7612071B2 (en) * 2004-03-12 2009-11-03 Syntrix Biosystems, Inc. Compositions and methods employing aminopterin
JP2008512490A (ja) * 2004-09-08 2008-04-24 チェルシー・セラピューティクス，インコーポレイテッド 異常細胞増殖および炎症の障害を治療するための代謝的に不活性な葉酸拮抗剤
WO2006074416A1 (en) * 2005-01-07 2006-07-13 Health Research Inc. 5-amino-4-imidazolecarboxamide riboside and its nucleobase as potentiators of antifolate transport and metabolism
WO2009126639A1 (en) * 2008-04-07 2009-10-15 Chelsea Therapeutics, Inc. Crystalline salt forms of antifolate compounds and methods of manufacturing thereof

Also Published As

Publication number Publication date
EP2300441A1 (en) 2011-03-30
WO2009126639A1 (en) 2009-10-15
BRPI0909198A2 (pt) 2019-09-24
CA2718330A1 (en) 2009-10-15
US20090253720A1 (en) 2009-10-08
US20090253719A1 (en) 2009-10-08
WO2009126637A1 (en) 2009-10-15
CN101981014A (zh) 2011-02-23
JP2011516561A (ja) 2011-05-26
MX2010010998A (es) 2011-01-25
EP2282740A1 (en) 2011-02-16
MX2010010999A (es) 2011-02-22
CA2718544A1 (en) 2009-10-15
JP2011516560A (ja) 2011-05-26
KR20100132061A (ko) 2010-12-16

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Legal Events

Date Code Title Description
MK4 Application lapsed section 142(2)(d) - no continuation fee paid for the application